(EN) Imidazolidyl macrolides of general structural formula (I) have been prepared from suitable precursors by alkylation and/or arylation at C-3'' and/or C-4'' of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.(FR) Cette invention concerne des macrolides d'imidazolidyle de formule structurelle générale (I). On a préparé ces macrolides d'imidazolidyle à partir de précurseurs appropriés, par alkylation et/ou arylation au niveau C-3'' et/ou C-4'' du cycle cyclohexyle. Ces immunodépresseurs à base de macrolides sont utiles chez un hôte mammifère pour traiter des maladies auto-immunes et des maladies infectieuses, et pour éviter le rejet des greffes d'organes étrangers et/ou les troubles, les maladies et les maux associés.
Imidazolidyl macrolides having immunosuppressive activity
申请人:MERCK & CO. INC.
公开号:EP0536896A1
公开(公告)日:1993-04-14
Imidazolidyl macrolides of the general structural Formula I:
have been prepared from suitable precursors by alkylation and/or arylation at C-3˝ and/or C-4˝ of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.
一般结构式 I 的咪唑烷基大环内酯:
由合适的前体通过环己基环的 C-3˝ 和/或 C-4˝ 烷基化和/或芳基化制备而成。这些大环内酯类免疫抑制剂可用于哺乳动物宿主治疗自身免疫性疾病、传染性疾病、预防外来器官移植的排斥反应和/或相关的痛苦、疾病和病症。
A colorimetric assay for screening transketolase activity
作者:Mark E.B. Smith、Ursula Kaulmann、John M. Ward、Helen C. Hailes
DOI:10.1016/j.bmc.2006.06.008
日期:2006.10
A tetrazolium red-based colorimetric assay has been devised to screen for transketolase activity with a range of aldehyde acceptors. The colorimetric TK assay is able to detect > 8% bioconversion using non-alpha-hydroxylated aldehydes as acceptor substrates and is significantly faster and more convenient to use than chromatographic procedures. (c) 2006 Elsevier Ltd. All rights reserved.
CANTRELL, THOMAS S.;ALLEN, ANDREW C., J. ORG. CHEM., 54,(1989) N, C. 135-139